US2003228366A1PendingUtilityA1

Reconstitutable compositions of biodegradable block copolymers

49
Priority: Jun 11, 2002Filed: Jun 11, 2002Published: Dec 11, 2003
Est. expiryJun 11, 2022(expired)· nominal 20-yr term from priority
Inventors:Chung ShihGaylen M. ZentnerAi-Zhi Piao
A61K 9/0019A61K 47/10A61K 47/14A61K 47/34
49
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Claims

Abstract

A composition having enhanced reconstitution properties and method of use is disclosed. The composition comprises one or more biodegradable block copolymer drug carriers; and a reconstitution enhancing and enabling agent comprising polyethylene glycol (PEG), a PEG derivative or a mixture of PEG and a PEG derivative; and wherein the biodegradable block copolymer drug carrier is soluble in an aqueous solution and in the liquid reconstitution enhancing and enabling agent.

Claims

exact text as granted — not AI-modified
We claim:  
     
         1 . A composition having enhanced reconstitution properties comprising: 
 1) one or more biodegradable block copolymer drug carriers comprising A-B, A-B-A or B-A-B block copolymers having a total weight average molecular weight of 2000 to 8000 Daltons, wherein the A block is a biodegradable polyester or poly(ortho ester) and the B block is polyethylene glycol(PEG), and the weight percentage of the A block is between 50.1% to 83% and the weight percentage of the B block is between 17% to 49.9%; and    2) a reconstitution enhancing and enabling agent comprising polyethylene glycol(PEG), a PEG derivative, or a mixtures of PEG and a PEG derivative, said PEG or PEG derivative having a molecular weight of 150 to 1100 Daltons;    wherein the biodegradable block copolymeric drug carrier is soluble in an aqueous solution and miscible with the reconstitution enhancing and enabling agent.    
     
     
         2 . The composition according to  claim 1  wherein the PEG derivative is comprised of PEG that has been derivatized with a member selected from the group consisting of D,L-lactide, D-lactide, L-lactide, D,L-lactic acid, D-lactic acid, L-lactic acid, glycolide, glycolic acid and copolymers thereof.  
     
     
         3 . The composition according to  claim 1  wherein the PEG derivative is represented by R 1 —CO—O-(PEG)-CO—R 2  or R 1 —O-(PEG)-R 2  wherein R 1  and R 2  are independently members selected from the group consisting of H and C 1  to C 10  alkyl.  
     
     
         4 . The composition according to  claim 1  wherein the biodegradable block copolymeric drug carrier further comprises a biodegradable polyester or poly(ortho ester) oligomer.  
     
     
         5 . The composition according to  claim 1  wherein the weight ratio of the biodegradable block copolymeric drug carrier and the reconstitution enhancing and enabling agent is within the range of 2:1 to 1:99.  
     
     
         6 . The composition according to  claim 1  further comprising a drug.  
     
     
         7 . The composition according to  claim 1 , wherein said composition can be reconstituted in water or an aqueous solution to form a homogeneous solution or an uniform colloidal system within 0.01 minutes to 180 minutes.  
     
     
         8 . A composition having enhanced reconstitution properties comprising: 
 1) one or more biodegradable ABA- or BAB-type tri-block copolymers comprising: 
 i) 51 to 83% by weight of a biodegradable, hydrophobic A block comprising a biodegradable polyester or poly(ortho ester), and  
 ii) 17 to 49% by weight of a hydrophilic B block comprising a polyethylene glycol(PEG), and wherein the tri-block copolymer having a weight average molecular weight of between about 2000 to 4990 and possessing reverse thermal gelation properties, and  
   2) a reconstitution enhancing and enabling agent comprising a polyethylene glycol(PEG), a PEG derivative, or a mixture of PEG and a PEG derivative, said PEG or PEG derivative having a weight averaged molecular weight of 150 to 1100 Daltons, and    wherein the biodegradable block copolymeric drug carrier is soluble in an aqueous solution and miscible with the reconstitution enhancing and enabling agent.    
     
     
         9 . The composition according to  claim 8  wherein the PEG derivative is comprised of PEG that has been derivatized with a member selected from the group consisting of D,L-lactide, D-lactide, L-lactide, D,L-lactic acid, D-lactic acid, L-lactic acid, glycolide, glycolic acid and copolymers thereof.  
     
     
         10 . The composition according to  claim 8  wherein the PEG derivative is represented by R 1 —CO—O-(PEG)-CO—R 2  or R 1 —O-(PEG)-R 2  wherein R 1  and R 2  are independently members selected from the group consisting of H and C 1  to C 10  alkyl.  
     
     
         11 . The composition according to  claim 8  wherein the biodegradable block copolymeric drug carriers further comprise a biodegradable polyester or poly(ortho ester) oligomer.  
     
     
         12 . The composition according to  claim 8  wherein the weight ratio of the biodegradable block polymeric drug carrier and the reconstitution enhancing and enabling agent is within the range of 2:1 to 1:99.  
     
     
         13 . The composition according to  claim 8  further comprising a drug.  
     
     
         14 . The composition according to  claim 8 , wherein said composition can be reconstituted in water or an aqueous solution to form a homogeneous solution or an uniform colloidal system within 0.01 minutes to 180 minutes  
     
     
         15 . A composition having enhanced reconstitution properties comprising: 
 1) a biodegradable ABA-type, BAB- or AB-type block copolymer, comprising: 
 i) 50.1 to 65% by weight of a biodegradable, hydrophobic A block comprising a biodegradable polyester or poly(ortho ester), and  
 ii) 35 to 49.9% by weight of a hydrophilic B block comprising a polyethylene glycol (PEG), and wherein the block copolymer has a weight average molecular weight of between 2400 to 4999 daltons, with the proviso that said block copolymer, when formed as an aqueous polymer solution, is a free flowing liquid at temperatures of between at least 35 to 42° C., and  
   2) a reconstitution enhancing and enabling agent comprising polyethylene glycol(PEG), a PEG derivative, or a mixture of PEG and a PEG derivative, said PEG or PEG derivative having a weight averaged molecular weight of 150 to 1100 Daltons, and    wherein the biodegradable block copolymeric drug carrier is soluble in an aqueous solution and miscible with the reconstitution enhancing and enabling agent.    
     
     
         16 . The composition according to  claim 15  wherein the PEG derivative is comprised of PEG that has been derivatized with a member selected from the group consisting of D,L-lactide, D-lactide, L-lactide, D,L-lactic acid, D-lactic acid, L-lactic acid, glycolide, glycolic acid and copolymers thereof.  
     
     
         17 . The composition according to  claim 15  wherein the PEG derivative is represented by R 1 —CO—O-(PEG)-CO—R 2  or R 1 —O-(PEG)-R 2  wherein R 1  and R 2  are independently members selected from the group consisting of H and C 1  to C 10  alkyl.  
     
     
         18 . The composition according to  claim 15  wherein the biodegradable block copolymeric drug carrier further comprises a biodegradable polyester or poly(ortho ester) oligomer.  
     
     
         19 . The composition according to  claim 15  wherein the weight ratio of the biodegradable block copolymeric drug carrier and the reconstitution enhancing and enabling agent is within the range of 2:1 to 1:99.  
     
     
         20 . The composition according to  claim 15  further comprising a drug.  
     
     
         21 . The composition according to  claim 15 , wherein said composition can be reconstituted in water or an aqueous solution to form a homogeneous solution or an uniform colloidal system within 0.01 minutes to 180 minutes  
     
     
         22 . A composition having enhanced reconstitution properties comprising: 
 1) a biodegradable polyester or poly(ortho ester) oligomer having a weight average molecular weight of between 400 and 10,000 daltons; and a biodegradable AB-type, ABA-type, or BAB-type block copolymer comprising: 
 i) 50.1 to 65% by weight of a biodegradable, hydrophobic A block comprising a biodegradable polyester or poly(ortho ester), and  
 ii) ii) 35 to 49.9% by weight of a hydrophilic B block comprising a polyethylene glycol (PEG), and wherein the block copolymer has a weight average molecular weight of between 2400 to 4999 daltons, and  
   2) a reconstitution enhancing and enabling agent comprising polyethylene glycol(PEG), a PEG derivative or a mixture of PEG and a PEG derivative, said PEG or PEG derivative having a weight averaged molecular weight of 150 to 1100 Daltons, and    wherein the biodegradable block copolymeric drug carrier is soluble in an aqueous solution and miscible with the reconstitution enhancing and enabling agent.    
     
     
         23 . The composition according to  claim 22  wherein the PEG derivative is comprised of PEG that has been derivatized with a member selected from the group consisting of D,L-lactide, D-lactide, L-lactide, D,L-lactic acid, D-lactic acid, L-lactic acid, glycolide, glycolic acid and copolymers thereof.  
     
     
         24 . The composition according to  claim 22  wherein the PEG derivative is represented by R 1 —CO—O-(PEG)-CO—R 2  or R 1 —O-(PEG)-R 2  wherein R 1  and R 2  are independently members selected from the group consisting of H and C 1  to C 10  alkyl.  
     
     
         25 . The composition according to  claim 22  wherein the biodegradable block copolymeric drug carrier further comprises a biodegradable polyester or poly(ortho ester) oligomer.  
     
     
         26 . The composition according to  claim 22  wherein the weight ratio of the biodegradable block copolymeric drug carrier and the reconstitution enhancing and enabling agent is within the range of 2:1 to 1:99.  
     
     
         27 . The composition according to  claim 22  further comprising a drug.  
     
     
         28 . The composition according to  claim 22 , wherein said composition can be reconstituted in water or an aqueous solution to form a homogeneous solution or an uniform colloidal system within 0.01 minutes to 180 minutes.  
     
     
         29 . A method of reconstituting a drug delivery composition comprising the steps of: 
 A) providing a composition having enhanced reconstitution properties comprising: 
 1) one or more biodegradable polymeric block copolymer drug carriers comprising A-B, A-B-A or B-A-B block copolymers having a total weight average molecular weight of 2000 to 8000 Daltons, wherein the A block is a biodegradable polyester or poly(ortho ester) and the B block is polyethylene glycol(PEG), and the weight percentage of the A block is between 50.1 to 83 and the weight percentage of the B block is between 17% to 49.9%; and  
 2) a reconstitution enhancing and enabling agent comprising a polyethylene glycol(PEG), a PEG derivative or a mixtures of PEG and a PEG derivative, said PEG or PEG derivative having a weight averaged molecular weight of 150 to 1100 Daltons;  
 wherein the biodegradable block copolymeric drug carrier is soluble in an aqueous solution and miscible with the liquid reconstitution enhancing and enabling agent; and  
   B) mixing water or an aqueous solution with the composition to form a homogeneous solution or an uniform colloidal system.    
     
     
         30 . The method according to  claim 29  wherein the PEG derivative is comprised of PEG that has been derivatized with a member selected from the group consisting of D,L-lactide, D-lactide, L-lactide, D,L-lactic acid, D-lactic acid, L-lactic acid, glycolide, glycolic acid and copolymers thereof.  
     
     
         31 . The method according to  claim 29  wherein the PEG derivative is represented by R 1 —CO—O-(PEG)-CO—R 2  or R 1 —O-(PEG)-R 2  wherein R 1  and R 2  are independently members selected from the group consisting of H and C 1  to C 10  alkyl.  
     
     
         32 . The method according to  claim 29  wherein the biodegradable drug block copolymeric carrier further comprises a biodegradable polyester or poly(ortho ester) oligomer.  
     
     
         33 . The method according to  claim 29  wherein the weight ratio of the biodegradable block copolymeric drug carrier and the reconstitution enhancing and enabling agent is within the range of 2:1 to 1:99.  
     
     
         34 . The method according to  claim 29 , wherein the composition further comprising a drug.  
     
     
         35 . The method according to  claim 29  wherein the ratio of the composition to water or aqueous solution is within the range of 2:1 to 1:1000.  
     
     
         36 . The method according to  claim 29  wherein the composition can be reconstituted in water or an aqueous solution to form a homogeneous solution or an uniform colloidal system within 0.01 minutes to 180 minutes.

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